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29 Cards in this Set
- Front
- Back
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physiologic effects of estrogen
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secondary sexual characteristics
reduces bone reabsorption enhances the coagulability of blood increases TG levels lowers LDL and increases HDL |
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adverse effects associated with estrogens
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thromboembolism
endometrial hyperplasia and cancer edema/weight gain HTN breakthrough bleeding |
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what can combination of P450 inducer and estrogen lead to
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breakthrough bleeding
reduce contraceptive efficacy |
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physiologic effects of progesterone
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increases insulin levels and response to glucose
enhance fat deposition decrease bone density decrease HDL |
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adverse effects of progestins
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glucose intolerance
decrease bone mineral density |
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3 selective estrogen receptor modulators (SERM)
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tamoxifen
raloxifene clomiphene |
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this SERM prevents receptor activation in breast cancer and agonist effect in bone, but cause endometrial hyperplasia
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tamoxifen
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this SERM is approved for prevention and treatment of osteoporosis with no effect on endometrial tissue
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raloxifene
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this SERM selectively blocks estrogen receptors in the pituitary reducing negative feedback to increase FSH and LH output
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clomiphene
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adverse effects associated with SERMs
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hot flashes
thromboembolism *endometrial thickening with tamoxifen |
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two competitive inhibitors of aromatase
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anastozole
letrozole |
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irreversible aromatase inhibitor
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exemestane
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adverse effects of aromatase inhibitors
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hot flashes
reduced bone mineral density |
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DOC for postmenopausal breast cancer
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aromatase inhibitors
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mechanism of axn of danazol
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weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors
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this drug is used in the treatment of endometriosis and fibrocystic disease of the breast
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danazol
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adverse effects in men and women with excess androgens
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women - virilization, hirsutism, deepened voice
men - paradixically result in feminization (gynecomastia, testicular shrinkage, infertility) due to feedback inhibition |
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adverse effects of high doses of anabolic steroids
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cholestatic jaundice
increased LFTs possibly hepatocellular carcinoma |
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oxandrolone
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anabolic steroid that increases the ratio of anabolic-to-androgenic activity
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5a-reducstase inhibitor
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finasteride
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nonsteroidal competitive inhibitor of adrogens at testosterone receptor
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flutamide
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adverse effects of flutamide
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gynecomastia
impotence hepatotoxicity |
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uses for flutamide
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prostate cancer
prevent effects of 1st dose of GnRH agonist treatment |
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this testosterone receptor antagonist has lower risk of hepatotoxicity
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bicalutamide
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mineralcorticoid receptor antagonist also has androgen-receptor antagonist activity; used for treatment of hirsutism
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spironolactone
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inhibition of cytochrome P450 enzymes involved in androgen synthesis
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ketoconazole
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clinical use for ketoconazole
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advanced prostate cancer that is resistant to first-line antiandrogen drugs
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uses for finasteride
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BPH
male pattern baldness |
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3 drugs that block androgen receptor
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flutamide
cyproterone spironolactone |
